ME02424B - ANTI-DESTROYING REVERSE - Google Patents

ANTI-DESTROYING REVERSE

Info

Publication number
ME02424B
ME02424B MEP-2016-95A MEP201695A ME02424B ME 02424 B ME02424 B ME 02424B ME P201695 A MEP201695 A ME P201695A ME 02424 B ME02424 B ME 02424B
Authority
ME
Montenegro
Prior art keywords
compound
subject
pharmaceutically acceptable
acceptable salt
use according
Prior art date
Application number
MEP-2016-95A
Other languages
German (de)
French (fr)
Unknown language (me)
Inventor
Solomon S Steiner
Bryan E Laulicht
Sasha H Bakhru
Edith Mathiowitz
Original Assignee
Perosphere Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47430065&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02424(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Perosphere Inc filed Critical Perosphere Inc
Publication of ME02424B publication Critical patent/ME02424B/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (23)

1. Jedinjenje formule II:ili njegova farmaceutski prihvatljiva so;gde su i L i L’ supstituisani ili nesupstituisani C1 do C10 alkilen lanac,gde su i M i M’ supstituisani C1 do C10 alkilen lanac i gde su i Y i Y’1. Compound of formula II: or a pharmaceutically acceptable salt thereof; where both L and L' are substituted or unsubstituted C1 to C10 alkylene chain, where both M and M' are substituted C1 to C10 alkylene chain and where both Y and Y' are 2. Jedinjenje prema patentnom zahtevu 1, naznačeno time što je jedinjenje predstavljeno formulom III: ili njegova farmaceutski prihvatljiva so.2. The compound according to claim 1, characterized in that the compound is represented by formula III: or its pharmaceutically acceptable salt. 3. Jedinjenje prema patentnom zahtevu 2, naznačeno time što je jedinjenje predstavljeno formulom IV: ili njegova farmaceutski prihvatljiva so, gde n je 3 do 5, m je 3 do 6 i G je izabran od -NH2 i OH.3. A compound according to claim 2, characterized in that the compound is represented by formula IV: or a pharmaceutically acceptable salt thereof, wherein n is 3 to 5, m is 3 to 6 and G is selected from -NH 2 and OH. 4. Jedinjenje prema patentnom zahtevu 3, naznačeno time što G je amino.4. The compound according to claim 3, characterized in that G is amino. 5. Jedinjenje prema patentnom zahtevu 1, naznačeno time što je jedinjenje predstavljeno formulom V ili njegova farmaceutski prihvatljiva so.5. The compound according to claim 1, characterized in that the compound is represented by formula V or a pharmaceutically acceptable salt thereof. 6. Jedinjenje prema patentnom zahtevu 1, naznačeno time što je jedinjenje predstavljeno formulom VI ili njegova farmaceutski prihvatljiva so.6. The compound according to claim 1, characterized in that the compound is represented by formula VI or a pharmaceutically acceptable salt thereof. 7. Jedinjenje prema patentnom zahtevu 1, naznačeno time što je jedinjenje predstavljeno formulom VII ili njegova farmaceutski prihvatljiva so.7. The compound according to claim 1, characterized in that the compound represented by formula VII or its pharmaceutically acceptable salt. 8. Jedinjenje prema patentnom zahtevu 1, naznačeno time što je jedinjenje predstavljeno formulom VIII ili njegova farmaceutski prihvatljiva so.8. The compound according to claim 1, characterized in that the compound is represented by formula VIII or a pharmaceutically acceptable salt thereof. 9. Farmaceutska kompozicija koja sadrži jedinjenje prema bilo kom od patentnih zahteva 1-8 i farmaceutski prihvatljiv nosač.9. A pharmaceutical composition containing a compound according to any one of claims 1-8 and a pharmaceutically acceptable carrier. 10. Farmaceutska kompozicija prema patentnom zahtevu 9, naznačena time što je kompozicija prilagođena (a) za enteralnu primenu; (b) za oralnu primenu; (c) za parenteralnu primenu; ili (d) za intravensku ili subkutanu primenu.10. Pharmaceutical composition according to patent claim 9, characterized in that the composition is adapted (a) for enteral administration; (b) for oral administration; (c) for parenteral administration; or (d) for intravenous or subcutaneous administration. 11. Jedinjenje prema bilo kom od patentnih zahteva 1-8 ili njegova farmaceutski prihvatljiva so za upotrebu u postupku potpune ili delimične reverzije antikoagulišućeg efekta inhibitora koagulacije kod subjekta kod koga postoji potreba za tim.11. A compound according to any of claims 1-8 or a pharmaceutically acceptable salt thereof for use in the process of complete or partial reversal of the anticoagulant effect of a coagulation inhibitor in a subject in need thereof. 12. Jedinjenje za upotrebu prema patentnom zahtevu 11, naznačeno time što je inhibitor koagulacije izabran iz grupe koja se sastoji od nefrakcionisanog heparina, heparina niske molekulske težine (LMWH), inhibitora faktora IIa i inhibitora faktora Xa.12. The compound for use according to claim 11, characterized in that the coagulation inhibitor is selected from the group consisting of unfractionated heparin, low molecular weight heparin (LMWH), factor IIa inhibitors and factor Xa inhibitors. 13. Jedinjenje za upotrebu prema patentnom zahtevu 12, naznačeno time što inhibitor koagulacije je inhibitor faktora Xa.13. The compound for use according to claim 12, characterized in that the coagulation inhibitor is a factor Xa inhibitor. 14. Jedinjenje za upotrebu prema patentnom zahtevu 13, naznačeno time što je inhibitor faktora Xa izabran iz grupe koja se sastoji od rivaroksabana, apiksabana, edoksabana i fondaparinuksa.14. The compound for use according to claim 13, characterized in that the factor Xa inhibitor is selected from the group consisting of rivaroxaban, apixaban, edoxaban and fondaparinux. 15. Jedinjenje za upotrebu prema patentnom zahtevu 11, naznačeno time što subjekat je (a) sisar; ili (b) čovek.15. The compound for use according to claim 11, characterized in that the subject is (a) a mammal; or (b) a human. 16. Jedinjenje za upotrebu prema patentnom zahtevu 11, naznačeno time što je potpuna ili delimična reverzija efekta antikoagulacije inhibitora koagulacije merena pomoću analize aktivnosti anti-faktora Xa.16. The compound for use according to claim 11, characterized in that the complete or partial reversal of the anticoagulation effect of the coagulation inhibitor is measured using an anti-factor Xa activity assay. 17. Jedinjenje za upotrebu prema patentnom zahtevu 11, naznačeno time što, subjekat kod koga postoji poptreba za tim je subjekat kod koga je indicirana akutna ili planirana reverzija antikoagulacije.17. The compound for use according to patent claim 11, characterized in that the subject in need of it is a subject in whom acute or planned reversal of anticoagulation is indicated. 18. Jedinjenje za upotrebu prema patentnom zahtevu 17, naznačeno time što (a) subjekat kod koga je indicirana akutna ili planirana reverzija antikoagulacije je subjekat koji pati od prekomerne doze antikoagulanta, subjekat koji pati od krvarenja, subjekat koji zahteva planiranu hiruršku intervenciju, subjekat koji se podvrgava invazivnoj ili neinvazivnoj proceduri koja zahteva biopsiju, subjekat koji se podvrgava proceduri u kojoj proceduralna greška može imati za rezultat krvarenje ako subjekat ostaje antikoagulisan, ili subjekat koji zahteva spinalnu ili epiduralnu anesteziju; ili (b) subjekat kod koga postoji potreba za tim je subjekat koji prima antikoagulaciju za prevenciju šloga, kardijačne hirurške i dijagnostičke postupke, srčane aritmije, prevenciju tromboze dubokih vena (DVT), plućne embolije ili generalno za prevenciju patoloških krvnih ugrušaka.18. The compound for use according to claim 17, characterized in that (a) the subject in whom acute or planned reversal of anticoagulation is indicated is a subject suffering from an overdose of anticoagulants, a subject suffering from bleeding, a subject requiring planned surgical intervention, a subject who is undergoing an invasive or non-invasive procedure requiring a biopsy, a subject undergoing a procedure in which a procedural error may result in bleeding if the subject remains anticoagulated, or a subject requiring spinal or epidural anesthesia; or (b) the subject in need of which is a subject receiving anticoagulation for the prevention of stroke, cardiac surgical and diagnostic procedures, cardiac arrhythmias, prevention of deep vein thrombosis (DVT), pulmonary embolism, or generally for the prevention of pathological blood clots. 19. Jedinjenje za upotrebu prema patentnom zahtevu 12, naznačeno time što inhibitor koagulacije je LMWH, i što je LMWH izabran iz grupe koja se sastoji od bemiparina, certoparina, dalteparina, enoksaparina, nadroparina, parnaparina, reviparina i tinzaparina.19. The compound for use according to claim 12, characterized in that the coagulation inhibitor is LMWH, and that the LMWH is selected from the group consisting of bemiparin, certoparin, dalteparin, enoxaparin, nadroparin, parnaparin, reviparin and tinzaparin. 20. Jedinjenje za upotrebu prema patentnom zahtevu 11, naznačeno time što se jedinjenje ili njegova farmaceutski prihvatljiva so primenjuje u masenom odnosu doze od između oko 0.01:1 do oko 1000:1 jedinjenja ili njegove farmaceutski prihvatljive soli prema antikoagulantu, poželjno što se jedinjenje ili njegova farmaceutski prihvatljiva so primenjuje u masenom odnosu doze od oko 10:1 jedinjenja ili njegove farmaceutski prihvatljive soli prema antikoagulantu.20. The compound for use according to claim 11, characterized in that the compound or its pharmaceutically acceptable salt is administered in a dose ratio by mass of between about 0.01:1 to about 1000:1 of the compound or its pharmaceutically acceptable salt to the anticoagulant, preferably the compound or its pharmaceutically acceptable salt is administered in a dose ratio of about 10:1 by weight of the compound or its pharmaceutically acceptable salt to the anticoagulant. 21. Jedinjenje za upotrebu prema patentnom zahtevu 11, naznačeno time što postupak sadrži primenu najmanje jednog dodatnog terapapeutskog sredstva; izborno što je najmanje jedno dodatno terapeutsko sredstvo vitamin K.21. Compound for use according to patent claim 11, characterized in that the procedure contains the application of at least one additional therapeutic agent; optionally, at least one additional therapeutic agent is vitamin K. 22. Dijagnostički kit koji sadrži jedinjenje prema bilo kom od patentnih zahteva 1-8.22. A diagnostic kit containing a compound according to any one of claims 1-8. 23. Kit prema patentnom zahtevu 22, naznačen time što se kit koristi za određivanje koncentracije antikoagulanta u krvi.23. The kit according to patent claim 22, characterized in that the kit is used to determine the concentration of anticoagulants in the blood.
MEP-2016-95A 2011-11-29 2012-11-29 ANTI-DESTROYING REVERSE ME02424B (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201161564559P 2011-11-29 2011-11-29
US201261614292P 2012-03-22 2012-03-22
US201261641698P 2012-05-02 2012-05-02
US201261666291P 2012-06-29 2012-06-29
EP12806229.6A EP2785700B1 (en) 2011-11-29 2012-11-29 Anticoagulant reversal agents
PCT/US2012/066938 WO2013082210A1 (en) 2011-11-29 2012-11-29 Anticoagulant reversal agents

Publications (1)

Publication Number Publication Date
ME02424B true ME02424B (en) 2016-09-20

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MEP-2016-95A ME02424B (en) 2011-11-29 2012-11-29 ANTI-DESTROYING REVERSE

Country Status (34)

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US (5) US9522892B2 (en)
EP (1) EP2785700B1 (en)
JP (1) JP6134731B2 (en)
KR (1) KR101892330B1 (en)
CN (1) CN104080772B (en)
AP (1) AP2014007662A0 (en)
AR (1) AR089020A1 (en)
AU (1) AU2012345975B2 (en)
BR (1) BR112014012892B1 (en)
CA (1) CA2856540C (en)
CL (1) CL2014001399A1 (en)
CO (1) CO6990738A2 (en)
CR (1) CR20140310A (en)
CY (1) CY1117414T1 (en)
DK (1) DK2785700T3 (en)
EA (1) EA027603B1 (en)
EC (1) ECSP14006696A (en)
ES (1) ES2569674T3 (en)
HR (1) HRP20160513T1 (en)
HU (1) HUE027452T2 (en)
IL (1) IL232788B (en)
ME (1) ME02424B (en)
MX (1) MX349514B (en)
PE (1) PE20141295A1 (en)
PH (1) PH12014501176B1 (en)
PL (1) PL2785700T3 (en)
PT (1) PT2785700E (en)
RS (1) RS54738B1 (en)
SG (1) SG11201402713WA (en)
SI (1) SI2785700T1 (en)
SM (1) SMT201600161B (en)
UA (1) UA116336C2 (en)
WO (1) WO2013082210A1 (en)
ZA (1) ZA201404793B (en)

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SG11201402713WA (en) 2014-06-27
EA201490823A1 (en) 2015-01-30
AU2012345975A1 (en) 2014-05-29
ES2569674T3 (en) 2016-05-12
SI2785700T1 (en) 2016-09-30
PH12014501176A1 (en) 2014-09-01
DK2785700T3 (en) 2016-06-13
CY1117414T1 (en) 2017-04-26
CL2014001399A1 (en) 2014-11-03
KR101892330B1 (en) 2018-08-27
SMT201600161B (en) 2016-07-01
ZA201404793B (en) 2015-04-29
EP2785700B1 (en) 2016-03-09
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